155062-48-9Relevant academic research and scientific papers
The discovery of MK-4256, a potent SSTR3 antagonist as a potential treatment of type 2 diabetes
He, Shuwen,Ye, Zhixiong,Truong, Quang,Shah, Shrenik,Du, Wu,Guo, Liangqin,Dobbelaar, Peter H.,Lai, Zhong,Liu, Jian,Jian, Tianying,Qi, Hongbo,Bakshi, Raman K.,Hong, Qingmei,Dellureficio, James,Pasternak, Alexander,Feng, Zhe,Dejesus, Reynalda,Yang, Lihu,Reibarkh, Mikhail,Bradley, Scott A.,Holmes, Mark A.,Ball, Richard G.,Ruck, Rebecca T.,Huffman, Mark A.,Wong, Frederick,Samuel, Koppara,Reddy, Vijay B.,Mitelman, Stan,Tong, Sharon X.,Chicchi, Gary G.,Tsao, Kwei-Lan,Trusca, Dorina,Wu, Margaret,Shao, Qing,Trujillo, Maria E.,Eiermann, George J.,Li, Cai,Zhang, Bei B.,Howard, Andrew D.,Zhou, Yun-Ping,Nargund, Ravi P.,Hagmann, William K.
supporting information; experimental part, p. 484 - 489 (2012/10/08)
A structure-activity relationship study of the imidazolyl-β- tetrahydrocarboline series identified MK-4256 as a potent, selective SSTR3 antagonist, which demonstrated superior efficacy in a mouse oGTT model. MK-4256 reduced glucose excursion in a dose-dependent fashion with maximal efficacy achieved at doses as low as 0.03 mg/kg po. As compared with glipizide, MK-4256 showed a minimal hypoglycemia risk in mice.
Route development and multikilogram GMP delivery of a somatostatin receptor antagonist
Ruck, Rebecca T.,Huffman, Mark A.,Stewart, Gavin W.,Cleator, Ed,Kandur, Wynne V.,Kim, Mary M.,Zhao, Dalian
, p. 1329 - 1337 (2012/10/29)
Route development and demonstration on multikilogram scale for the first GMP delivery of MK-4256 are described. Key aspects of the convergent route include a regioselective green iodination, one-pot oxadiazole synthesis, and an efficient ketone Pictet-Spengler reaction with diastereomeric upgrade via crystallization to afford 6 kg of API. A recycle procedure augmented the yield of desired diastereomer in the Pictet-Spengler reaction from a mixture of diastereomers heavily enriched in the undesired diastereomer.
Substituted sulphonyl amino(thio)carbonyl compounds and their use as herbicides
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Page column 53, (2010/11/30)
The invention relates to novel sulfonylamino(thio)carbonyl compounds of the formula (I), in whichn represents the numbers 0, 1 or 2,A represents a single bond, or oxygen or sulfur, or the grouping N—R, in which R represents hydrogen, alkyl, alkenyl, alkin
